Table 1. CK2 Biochemical and Cellular Potency for Compounds 7a–l.
| compd | CK2α IC50 (nM)a | pAKTS129 IC50 (nM)a | HCT-116 GI50 (nM)a | sol. (μM)a | LogDa | Hu PPB (% free)a | microsomal stabilityb | hERG IC50 (μM) |
|---|---|---|---|---|---|---|---|---|
| 7a | <3 | ND | 300 | <1 | 3.1 | 3 | 22 | >33 |
| 7b | <3 | 2 | 81 | 8 | 2.4 | 8 | 15 | 21 |
| 7c | <3 | ND | 67 | <1 | 3.0 | 4 | 56 | >33 |
| 7d | <3 | 3 | 21 | <1 | 3.1 | 2 | 39 | 19 |
| 7e | <3 | 2 | 57 | 5 | 2.3 | 13 | 36 | 16 |
| 7f | <3 | 2 | 12 | 7 | 2.8 | 9.6 | 19 | ND |
| 7g | <3 | 42 | ND | 18 | 2.1 | 15 | 50 | >33 |
| 7h | <3 | 6 | 300 | 7 | 2.1 | 12 | <4 | 19 |
| 7i | <3 | 33 | 600 | <1 | 2.9 | 2.4 | 47 | 11 |
| 7j | <3 | 8 | 410 | 5 | 3.0 | 4.3 | 31 | 16 |
| 7k | <3 | 3 | ND | 1 | 2.1 | 12 | <4 | ND |
| 7l | <3 | 10 | 110 | 52 | 0.8 | 21 | 20 | ND |
a
Mean value of two experiments. Deviations were within < ±25%.
b
Intrinsic clearance (CLint) determined from rat liver microsome incubations (μL/min/mg); ND = not determined.